INCB053914

INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively; INCB053914 is highly selective against a panel of more than 50 kinases (>475-fold selectivity) with exception of RSK2 (IC50=7.1 uM); inhibits cellular proliferation in a panel of cell lines derived from hematologic malignancies including AML, MM, DLBCL, MCL, and T-ALL with GI50 of <100 nM, inhibits proliferation in all MM cell lines with GI5050 of 13.2-230.0 nM; inhibits PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells with IC50 of 4 and 27 nM, also increases PIM2 expression in KG-1a (AML), Pfeiffer, and KMS12-PE cells; in vivo, INCB053914 inhibited Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts. Solid Tumors Phase 2 Clinical

References 1. Koblish H, et al. PLoS One. 2018 Jun 21;13(6):e0199108. View Related Products by Target Pim Solid Tumors